Search PubMed⌕ Search

PubMed · 15988604

[Haemostaseology].

Abstract

The design and development of new antithrombotics, i.e. anticoagulants and antiplatelet drugs, is a rapidly expanding area of pharmacological research. New anticoagulants, i.e. inhibitors of thrombin formation and action have been developed and some of them are already in clinical use. This includes hirudin and its analogs, such as bivalirudin. In contrast to heparins, these compounds as well as low-molecular weight inhibitors of thrombin and factor Xa directly inhibit thrombus-associated generation and action of thrombin, eventually associated with a reduced bleeding tendency. Orally active compounds are available and currently subject of clinical trials. It appears possible that these new agents may replace cumarins as oral anticoagulants, specifically in long-term use, in the near future. The introduction of clopidogrel marks another important development in the field of antiplatelet drugs. Synergistic actions of this compound with acetylsalicylic acid and GP-IIb/IIIa-antagonists because of their different mode of action enhance the antithrombotic potential considerably and have been clinically confirmed. Despite of this optimistic outlook, the individual risk/benefit ratio of these new drugs, in particular in the area of anticoagulants, still needs to be defined.

Explore related subjects

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

K Schrör. 2005. [Haemostaseology].. https://doi.org/10.1007/s00108-005-1452-3

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

Microparticles and nanoparticles for drug delivery.

Particulate drug delivery systems have become important in experimental pharmaceutics and clinical medicine. The distinction is often made between micro- and nanoparticles, being particles with dimensions best described in micrometers and nanometers respectively. That size difference entails real differences at many levels, from formulation to in vivo usage. Here I will discuss those differences and provide examples of applications, for local and systemic drug delivery. I will outline a number of challenges of interest in particulate drug delivery.

Drug Delivery Systems↗

On the suitability of nanocrystalline ferrites as a magnetic carrier for drug delivery: functionalization, conjugation and drug release kinetics.

Superparamagnetic nickel ferrite nanoparticles functionalized with polyvinyl alcohol, polyethylene oxide and polymethacrylic acid (PMAA) polymers and subsequently conjugated with doxorubicin anti-cancer drug are studied for their use as a magnetic carrier for drug delivery. Fourier transform infrared spectroscopy enabled examination of the ability of the nanoparticles to be functionalized with polymers and conjugated with doxorubicin drug. The functionalized polymer-coated nanocrystalline nickel ferrites retain the magnetic characteristics of non-functionalized nanocrystalline nickel ferrites (superparamagnetism, absence of hysteresis, remanence and coercivity at room temperature), encouraging their application as a magnetic carrier for drug delivery. The PMAA-coated nanoferrites are demonstrated as being a potentially superior magnetically targeted drug carrier based on FTIR results and drug release kinetics in the absence and presence of an external magnetic field.

Drug Delivery Systems↗

Internalization of novel non-viral vector TAT-streptavidin into human cells.

BACKGROUND: The cell-penetrating peptide derived from the Human immunodeficiency virus-1 transactivator protein Tat possesses the capacity to promote the effective uptake of various cargo molecules across the plasma membrane in vitro and in vivo. The objective of this study was to characterize the uptake and delivery mechanisms of a novel streptavidin fusion construct, TAT47-57-streptavidin (TAT-SA, 60 kD). SA represents a potentially useful TAT-fusion partner due to its ability to perform as a versatile intracellular delivery vector for a wide array of biotinylated molecules or cargoes. RESULTS: By confocal and immunoelectron microscopy the majority of internalized TAT-SA was shown to accumulate in perinuclear vesicles in both cancer and non-cancer cell lines. The uptake studies in living cells with various fluorescent endocytic markers and inhibiting agents suggested that TAT-SA is internalized into cells efficiently, using both clathrin-mediated endocytosis and lipid-raft-mediated macropinocytosis. When endosomal release of TAT-SA was enhanced through the incorporation of a biotinylated, pH-responsive polymer poly(propylacrylic acid) (PPAA), nuclear localization of TAT-SA and TAT-SA bound to biotin was markedly improved. Additionally, no significant cytotoxicity was detected in the TAT-SA constructs. CONCLUSION: This study demonstrates that TAT-SA-PPAA is a potential non-viral vector to be utilized in protein therapeutics to deliver biotinylated molecules both into cytoplasm and nucleus of human cells.

Drug Delivery Systems↗